ChEMBL ligand: CHEMBL41036
Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827] There should be some charts here, you may need to enable JavaScript!
Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Thyroid hormone receptor-α/Thyroid hormone receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1860] [GtoPdb: 588] [UniProtKB: P10827]
ChEMBL	Displacement of [125I]3,5,3'-triiodo-L-thyronine from His-tagged human recombinant TRalpha1 by scintillation proximity assay	B	8.11	pKi	7.79	nM	Ki	J Med Chem (2008) 51: 7075-7093 [PMID:18975928]
ChEMBL	Displacement of [125I]T3 from recombinant thyroid hormone receptor alpha expressed in sf9 cells by scintillation proximity assay	B	8.14	pKi	7.18	nM	Ki	Proc Natl Acad Sci U S A (2007) 104: 15490-15495 [PMID:17878314]
ChEMBL	Binding affinity to TRalpha1	B	8.14	pKi	7.18	nM	Ki	J Med Chem (2012) 55: 5649-5675 [PMID:22512468]
ChEMBL	Inhibition of thyroid hormone receptor alpha	B	7.6	pIC50	25.12	nM	IC50	Bioorg Med Chem (2007) 15: 4609-4617 [PMID:17467994]
GtoPdb	-	-	7.6	pIC50	-	-	-	J Med Chem (2003) 46: 1580-8 [PMID:12699376]
ChEMBL	Concentration required to inhibit 50% of I-T3 binding to hTR1 (Thyroid hormone receptor alpha) was determined	B	7.6	pIC50	25	nM	IC50	J Med Chem (2003) 46: 1580-1588 [PMID:12699376]
ChEMBL	Inhibitory concentration against cloned human thyroid hormone receptor alpha 1	B	7.6	pIC50	25	nM	IC50	Bioorg Med Chem Lett (2005) 15: 4579-4584 [PMID:16099653]
ChEMBL	Binding affinity at human thyroid hormone receptor alpha 1 expressed in CHOK1 cells	B	7.6	pIC50	25	nM	IC50	Bioorg Med Chem Lett (2007) 17: 4131-4134 [PMID:17543524]
ChEMBL	Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor alpha (TRalpha1) and an alkaline phosphate reporter gene downstream thyroid response element TRAF-alpha1 was determined	B	7.96	pEC50	11	nM	EC50	J Med Chem (2003) 46: 1580-1588 [PMID:12699376]
ChEMBL	Agonist activity at recombinant His6-tagged THR-alpha (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay	B	8.3	pEC50	5	nM	EC50	J Med Chem (2014) 57: 3912-3923 [PMID:24712661]
ChEMBL	Agonist activity at human thyroid hormone receptor alpha expressed in CV1 cells by TRE-luciferase assay	F	8.35	pEC50	4.5	nM	EC50	Bioorg Med Chem Lett (2008) 18: 3919-3924 [PMID:18585912]
Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828]
ChEMBL	Displacement of [125I]T3 from recombinant thyroid hormone receptor beta expressed in sf9 cells by scintillation proximity assay	B	9.43	pKi	0.37	nM	Ki	Proc Natl Acad Sci U S A (2007) 104: 15490-15495 [PMID:17878314]
ChEMBL	Binding affinity to TRbeta1	B	9.43	pKi	0.37	nM	Ki	J Med Chem (2012) 55: 5649-5675 [PMID:22512468]
ChEMBL	Displacement of [125I]3,5,3'-triiodo-L-thyronine His-tagged human recombinant TRbeta1 by scintillation proximity assay	B	9.62	pKi	0.24	nM	Ki	J Med Chem (2008) 51: 7075-7093 [PMID:18975928]
ChEMBL	Concentration required to inhibit 50% of I-T3 binding to hTR1 (Thyroid hormone receptor beta) was determined	B	8.96	pIC50	1.1	nM	IC50	J Med Chem (2003) 46: 1580-1588 [PMID:12699376]
ChEMBL	Inhibitory concentration against cloned human thyroid hormone receptor beta 1	B	8.96	pIC50	1.1	nM	IC50	Bioorg Med Chem Lett (2005) 15: 4579-4584 [PMID:16099653]
ChEMBL	Binding affinity at human thyroid hormone receptor beta-1 expressed in CHOK1 cells	B	8.96	pIC50	1.1	nM	IC50	Bioorg Med Chem Lett (2007) 17: 4131-4134 [PMID:17543524]
GtoPdb	-	-	8.96	pIC50	-	-	-	Proc Natl Acad Sci USA (2003) 100: 10067-72 [PMID:12888625]
ChEMBL	Inhibition of human thyroid hormone receptor beta 1	B	8.96	pIC50	1.1	nM	IC50	Bioorg Med Chem (2007) 15: 5251-5261 [PMID:17524652]
ChEMBL	Inhibition of thyroid hormone receptor beta	B	8.96	pIC50	1.1	nM	IC50	Bioorg Med Chem (2007) 15: 4609-4617 [PMID:17467994]
ChEMBL	Agonist activity at recombinant His6-tagged THR-beta (unknown origin) expressed in Escherichia coli BL21(DE3) co-expressing RXR preincubated for 30 mins assessed as biotin-GRIP1 peptide recruitment by HTRF assay	B	7.64	pEC50	23	nM	EC50	J Med Chem (2014) 57: 3912-3923 [PMID:24712661]
ChEMBL	Effect on CHO-K1 cells stably transfected with Thyroid hormone receptor beta and an alkaline phosphate reporter gene downstream thyroid response element TRAF-beta1 was determined	B	8.46	pEC50	3.5	nM	EC50	J Med Chem (2003) 46: 1580-1588 [PMID:12699376]
ChEMBL	Agonist activity at human thyroid hormone receptor beta expressed in CV1 cells by TRE-luciferase assay	F	8.95	pEC50	1.12	nM	EC50	Bioorg Med Chem Lett (2008) 18: 3919-3924 [PMID:18585912]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]